哌啶链接1,2,3-三氮唑化合物的合成及抗细菌活性  

Synthesis and antibacterial evaluation of piperidin linked with 1,2,3-triazole derivatives

作　　者：贾淑红[1] 李翠平 何兴[1] 毛龙飞[1] 徐桂清[1] 

机构地区：[1]河南师范大学化学化工学院,河南新乡453007 [2]天方药业有限公司,河南驻马店463000

出　　处：《化学研究与应用》2016年第2期158-163,共6页Chemical Research and Application

摘　　要：以丙二酸环异丙酯为起始原料,通过酯化生成甲酰乙酸叔丁酯衍生物(2a-2e);2再与4-叠氮基-1-Boc基哌啶在碳酸钾催化下经"点击反应"生成Boc-哌啶链接1,2,3-三氮唑衍生物(3a-3e);3在三氟乙酸作用下脱Boc基团,生成一系列新型哌啶链接1,2,3-三氮唑化合物(4a-4e)。所得到的5种化合物均未有文献报道,结构通过1H NMR,ESI-MS和元素分析进行表征。生物活性测试结果表明,五种化合物均有良好的抗细菌活性。Formyl tertiary butyl acetate derivatives（ 2a-2e） were synthesized through esterification from 2,2-dimethyl-1,3-dioxane-4,6-dione.1-（ Piperidin-4-Boc）-1H-1,2,3-triazole derivatives（ 3a-3e） were designed and obtained via click reactions by compounds（ 2a-2e） and 4-azide-1-Boc-piperidine using K2CO3 as the catalyst.A series of new 1-（ piperidin-4-yl）-1H-1,2,3-triazole derivatives（ 4a-4e） were synthesized under trifluoroacetic acid by taking off the Boc group on compounds（ 3a-3e）. Five compounds were characterized by1 H NMR and ESI-MS.Biological activity test showed that all these compounds displayed good antibacterial activity.

关 键 词：丙二酸环异丙酯 “点击反应” 哌啶 1 2 3-三氮唑 抗细菌活性 

分 类 号：O626.2[理学—有机化学]